Bioactive Small Molecules
Cayman Chemical Picrotin, Purity: ≥98%, CAS: 21416-53-5, 100 mg
A natural antagonist of GlyRs (IC50s = 57 and 117 µM for α1 and α2 homodimeric GlyRs, respectively); does not inhibit GABAA or GABAC receptors
Cayman Chemical CJ-13610, Purity: ≥98%, CAS: 179420-17-8, 10 mg
An inhibitor of 5-LO (IC50 = 70 nM for 5-LO product formation in A23187-challenged PMNLs); inhibits recombinant 5-LO in a glutathione peroxidase-dependent manner (IC50 = 300 nM); reduces levels of LTB4 and decreases mechanical hyperalgesia in a rat model of chronic inflammatory pain induced by Freund's adjuvant (3-10 mg/kg); reverses tactile allodynia and increases hind paw weight bearing in a rat medial meniscal transection model of osteoarthritic pain (0.6-6 mg/kg)
Medchemexpress LLC Cis-piperidine-2,3-dicarboxylic acid | 46026-75-9 | >98.0% | 50 MG
Cis-piperidine-2,3-dicarboxylic acid is a research reagent that modulates ionotropic glutamate receptors. It functions as a non-specific antagonist of NMDA, AMPA, and kainate receptors and as a partial agonist at NMDA receptors, and is used to block or study excitatory synaptic transmission in neuropharmacology experiments.
- Acts as a non-specific antagonist of NMDA, AMPA, and kainate receptors.
- Exhibits partial agonist activity at NMDA receptors for modulation studies.
- High purity (≥98.0%) suitable for research applications.
- Soluble in water (≈100 mg/mL) with ultrasonic assistance.
- Off-white to light yellow solid stored at 4°C and protected from light.
Selleck Chemical LLC Pexidartinib Hydrochloride E6007-100MG
Pexidartinib Hydrochloride is an oral tyrosine kinase inhibitor of colony-stimulating factor 1 receptor (CSF1R) It significantly reduces macrophage levels in adipose tissue without altering overall myeloid cell counts in mice It also induces developmental and immunotoxic effects in zebrafish embryos by hyperactivating Wnt signaling
Apexbio Technology LLC (+)-MK 801(Synonyms: Dizocilpine, Dizocilpine maleate, MK-801, (+)-MK-801, (+)-Dizocilpine), 10mg, CAS: 70449-94-4.
( )-MK 801 (CAS 70449-94-4) is a potent selective and non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor displaying a Ki of approximately 30 5 nM This small molecule readily crosses the blood-brain barrier and interacts reversibly with specific binding sites on cortical membranes predominantly localized within the hippocampus In vitro assays utilizing rat cortical slice preparations indicate that ( )-MK 801 robustly inhibits NMDA-induced depolarization events and suppresses epileptiform activity mediated by neurotoxic agents Due to these pharmacological properties ( )-MK 801 is utilized experimentally in neuroscience research to study NMDA receptor-mediated events neurotoxicity convulsions and excitatory neurotransmission pathways
Medchemexpress LLC 2-(methylamino)-1H-purin-6(7H)-one (N2-methylguanine) | 10030-78-1 | MFCD00127896 | 98.0% | 165.15 g/mol | C6H7N5O | 100 MG
2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) is a modified purine nucleobase and endogenous methylated nucleoside supplied as a solid research reagent. It is used as a reference standard and analytical reagent in studies of nucleic acid modification, enzymology, and biomarker analysis.
- Modified purine nucleobase relevant to nucleic acid research.
- High purity suitable for analytical and biochemical assays.
- Available in multiple milligram-scale sizes for experimental flexibility.
- Solid physical form for straightforward handling and storage.
- Suitable as a reference standard for modification and biomarker studies.
AdipoGen Darunavir . ethanolate (250 mg)
Chemical. CAS: 635728-49-3. Formula: C27H37N3O7S . C2H5OH. MW: 547.7 . 46.0. Darunavir ethanolate is a highly potent HIV protease inhibitor (IC50=3-6nM, depending on laboratory HIV-1 strain), an antiretroviral medication used to treat and prevent HIV/AIDS. The ethanolate formulation has some stability advantages compared to the free base Darunavir (Prod. No. AG-CR1-3712). Darunavir ethanolate is a second generation HIV-1 protease inhibitor that inhibits replication of various laboratory strains and clinical isolates of HIV-1, including those resistant to first generation protease inhibitors. It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations. Formulations containing darunavir have been used in combination therapy for the treatment of HIV. Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the papain like viral protease (PLVP) of SARS-CoV-2, responsible for COVID-19.
Cayman Chemical NNC 55-0396, Purity: ≥95%, CAS: 357400-13-6, 5 mg
A selective inhibitor of T-type calcium channels (IC50 = 6.8 μM); exhibits no activity against L-type calcium channels up to 100 μM; inhibits tremor in mice (20 mg/kg and 12.5 mg/kg in GABAA α1-null and harmaline-induced tremor models, respectively); inhibits Kv channels (IC50 = 80 nM)
TARGETMOL CHEMICALS INC DYNAMIN IN-2 5MG
Also available in 1 mg 10 mg 25 mg 50 mg 100 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Dynamin IN-2 (compound 43) is a Wiskostatin analogue. Dynamin IN-2 is a potent dynamin inhibitor (dynamin I GTPase IC50= 1.0 uM). Dynamin IN-2 blocks clathrin mediated endocytosis (CME) (IC50= 9.5 uM). purity: 98%
Cayman Chemical FX1, Purity: ≥95%, CAS: 1426138-42-2, 10 mg
A BCL6 inhibitor (IC50 = ~35 μM); selective for BCL6 over a panel of 50 kinases at 10 μM; reduces recruitment of the BCL6 corepressor proteins SMRT and BCOR to the BCL6 target loci CDKN1A, CD69, and CXCR4 in a ChIP assay at 50 μM; represses growth of Farage, SU-DLH-6, DOHH-2, OCI-Ly7, RCK8, SU-DHL-4, OCI-Ly1, and SC-1 BCL6-dependent cell lines (GI50s = 16-54 μM); reduces tumor volume in an HBL-1 large B cell lymphoma mouse xenograft model at 50 mg/kg
STEMCELL Technologies BIRB-796, Size: 10 mg
BIRB-796 is a highly potent inhibitor of p38 MAPK (Kd = 0.1 nM) that blocks TNFα release in LPS-stimulated THP-1 cells (IC₅₀ = 18 nM) (Pargellis et al.). At 10 μM, BIRB-796 can also inhibit JNK2α2 in vitro, but at lower concentrations BIRB-796 inhibits p38 MAPK without affecting phosphorylation of JNK substrates (Bain et al.; Kuma et al.).MAINTENANCE AND SELF-RENEWAL· Rescues the self-renewal ability of muscle satellite cells from aged mice (Bernet et al.).· Increases the regenerative capacity of functional aged skeletal muscle stem cells grown in hydrogel (Cosgrove et al.).· Blocks GADD45G-induced differentiation of long-term repopulating hematopoietic stem cells (Thalheimer et al.).· Enhances stem cell activity of cultured umbilical cord blood-derived hematopoietic cells cultured in serum-free medium supplemented with SCF, TPO, and FLT3L (Baudet et al.).· Blocks the osteogenic differentiation effect of myocilin on human mesenchymal stem cells (Kwon et al.).
Medchemexpress LLC Azido-PEG1 | 1517-05-1 | 100.0% | 87.08 | 100 MG
Azido-PEG1 is a versatile PEG-based PROTAC linker primarily utilized for synthesizing PROTACs. Its core feature is an azide group, which makes it a potent click chemistry reagent. This allows it to readily engage in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules that possess alkyne groups and can also participate in strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- PEG-based PROTAC linker
- Enables the synthesis of PROTACs
- Functions as a click chemistry reagent
- Contains an azide group
- Capable of copper-catalyzed azide-alkyne cycloaddition (CuAAc)
- Capable of strain-promoted alkyne-azide cycloaddition (SPAAC)
- Versatile reactivity
Medchemexpress LLC Tolebrutinib | 1971920-73-6 | 99.8% | 455.51 | 1 MG
Tolebrutinib (SAR442168) is a potent, selective, orally active, and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. It exhibits efficacy in central nervous system immunity and can be used for the research of multiple sclerosis (MS).
- Potent, selective, orally active, and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK).
- Exhibits efficacy in central nervous system immunity.
- Can be used for the research of multiple sclerosis (MS).
- High purity: 99.79%.
Medchemexpress LLC Benzamide, 5-chloro-4-[(3,4-dichlorophenoxy)methyl]-2-fluoro-N-(methylsulfonyl)- | 1355631-24-1 | 99.4% | 426.67 | 1 ML
Nav1.7 inhibitor (compound II) is a potent sulfonamide Nav1.7 inhibitor. It has potential for treating various pain disorders, including acute, inflammatory, and neuropathic pain.
- Potent Nav1.7 inhibitor
- Purity 99.4%
- Molecular weight 426.67
- CAS number 1355631-24-1
- Formula C15H11Cl3FNO4S
- Appearance is solid, white to off-white
- Shipping at room temperature in continental US; may vary elsewhere
- Storage for powder at -20°C for 3 years, 4°C for 2 years
- Storage for in solvent at -80°C for 2 years, -20°C for 1 year
- Solubility (in vitro): ≥ 100 mg/mL (234.37 mM) in DMSO
- Solubility (in vivo): ≥ 2.5 mg/mL (5.86 mM) in 10% DMSO and 90% corn oil
- Target Nav1.7
Medchemexpress LLC Betrixaban maleate | 936539-80-9 | MFCD31729381 | 99.8% | 567.98 g/mol | C27H26ClN5O7 | 25 MG
Betrixaban maleate is the maleate salt of betrixaban, a potent and selective orally active factor Xa (fXa) inhibitor used as a research compound to study coagulation and antithrombotic pharmacology. The compound is supplied as a high-purity research chemical suitable for in vitro and in vivo experiments.
- High purity suitable for research (99.78%).
- Maleate salt improves handling and solubility properties.
- Targets factor Xa for antithrombotic studies.
- Molecular weight 567.98 g/mol; formula C27H26ClN5O7.
- Available in small milligram quantities for laboratory use (e.g., 25 mg).
- Supplied for research use only; not for human or clinical applications.